EP2295550A3 - Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen und deren Verwendung - Google Patents

Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen und deren Verwendung Download PDF

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Publication number
EP2295550A3
EP2295550A3 EP10011814A EP10011814A EP2295550A3 EP 2295550 A3 EP2295550 A3 EP 2295550A3 EP 10011814 A EP10011814 A EP 10011814A EP 10011814 A EP10011814 A EP 10011814A EP 2295550 A3 EP2295550 A3 EP 2295550A3
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EP
European Patent Office
Prior art keywords
gsk
protein
relates
methods
inhibitors
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP10011814A
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English (en)
French (fr)
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EP2295550A2 (de
Inventor
Ernst Ter Haar
Lovorka Swenson
Jeremy Green
Michael J. Arnost
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of EP2295550A2 publication Critical patent/EP2295550A2/de
Publication of EP2295550A3 publication Critical patent/EP2295550A3/de
Withdrawn legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10Transferases (2.)
    • C12N9/12Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/30Drug targeting using structural data; Docking or binding prediction
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2299/00Coordinates from 3D structures of peptides, e.g. proteins or enzymes
    • GPHYSICS
    • G16INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16BBIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Spectroscopy & Molecular Physics (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Theoretical Computer Science (AREA)
  • Medical Informatics (AREA)
  • Evolutionary Biology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Microbiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
EP10011814A 2001-04-30 2002-04-29 Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen und deren Verwendung Withdrawn EP2295550A3 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US28736601P 2001-04-30 2001-04-30
US29709401P 2001-06-08 2001-06-08
US36189902P 2002-02-27 2002-02-27
EP09004787A EP2082743A3 (de) 2001-04-30 2002-04-29 Inhibitoren von GSK-3 und Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen
EP02729056A EP1435957B1 (de) 2001-04-30 2002-04-29 Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
EP02729056.8 Division 2002-04-29
EP09004787.9 Division 2009-03-31

Publications (2)

Publication Number Publication Date
EP2295550A2 EP2295550A2 (de) 2011-03-16
EP2295550A3 true EP2295550A3 (de) 2011-12-14

Family

ID=27403701

Family Applications (3)

Application Number Title Priority Date Filing Date
EP10011814A Withdrawn EP2295550A3 (de) 2001-04-30 2002-04-29 Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen und deren Verwendung
EP02729056A Expired - Lifetime EP1435957B1 (de) 2001-04-30 2002-04-29 Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen
EP09004787A Withdrawn EP2082743A3 (de) 2001-04-30 2002-04-29 Inhibitoren von GSK-3 und Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen

Family Applications After (2)

Application Number Title Priority Date Filing Date
EP02729056A Expired - Lifetime EP1435957B1 (de) 2001-04-30 2002-04-29 Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen
EP09004787A Withdrawn EP2082743A3 (de) 2001-04-30 2002-04-29 Inhibitoren von GSK-3 und Kristallstrukturen von GSK-3-beta-Protein und -Proteinkomplexen

Country Status (9)

Country Link
US (4) US7390808B2 (de)
EP (3) EP2295550A3 (de)
JP (2) JP2005504731A (de)
AT (1) ATE433751T1 (de)
AU (1) AU2002259071A1 (de)
CA (1) CA2444882A1 (de)
DE (1) DE60232669D1 (de)
MX (1) MXPA03009957A (de)
WO (1) WO2002088078A2 (de)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002024893A2 (en) * 2000-09-19 2002-03-28 Chiron Corporation CHARACTERIZATION OF THE GSK-3β PROTEIN AND METHODS OF USE THEREOF
KR20040084896A (ko) * 2002-02-06 2004-10-06 버텍스 파마슈티칼스 인코포레이티드 Gsk-3의 억제제로서 유용한 헤테로아릴 화합물
JP2005532265A (ja) * 2002-02-11 2005-10-27 カイロン コーポレイション ヒトgsk3を結晶化するための方法およびその新規な結晶構造
AU2003245700A1 (en) * 2002-02-12 2003-09-04 Glaxo Group Limited Pyrazolopyridine derivatives
GB0207249D0 (en) * 2002-03-27 2002-05-08 Glaxo Group Ltd Novel compounds
EP1627323A4 (de) * 2003-05-06 2008-04-09 New Century Pharmaceuticals Albumin-bindestellen zur bewertung von medikamentenwechselwirkungen und verfahren zur bewertung oder entwicklung von medikamenten auf der basis ihrer albumin-bindeeigenschaften
WO2005035532A1 (en) * 2003-10-10 2005-04-21 Pfizer Products Inc. Substituted 2h-[1,2,4]triazolo[4,3-a]pyrazines as gsk-3 inhibitors
EP1684705A4 (de) * 2003-11-03 2008-02-20 New Century Pharmaceuticals Albumin-bindungsstellen zur beurteilung von arzneimittelwechselwirkungen und verfahren zur beurteilung oder zum entwurf von arzneimitteln auf basis ihrer albuminbindungseigenschaften
EP1723427A2 (de) * 2004-02-26 2006-11-22 Bayer HealthCare AG Diagnostika und therapeutika für mit glycogen-synthase-kinase 3 beta (gsk3b) in zusammenhang stehende krankheiten
ATE427499T1 (de) * 2004-05-21 2009-04-15 Inst Systems Biology Zusammensetzungen und verfahren zur quantifizierung von serumglykoproteinen
ES2386027T3 (es) * 2004-10-29 2012-08-07 Abbott Laboratories Inhibidores de quinasas novedosos
WO2009126335A2 (en) * 2008-04-08 2009-10-15 University Of Florida Research Foundation, Inc. Ant2 inhibitor compounds and methods of use thereof
US20100016247A1 (en) * 2008-07-21 2010-01-21 Florida State University Research Foundation Using budding yeast to screen for inhibitors of aurora kinases
US20110230564A1 (en) * 2008-08-01 2011-09-22 University Of Florida Research Foundation Ant4 inhibitor compounds and methods of use thereof
WO2010027458A2 (en) * 2008-09-02 2010-03-11 University Of Florida Research Foundation, Inc. Pdk inhibitor compounds and methods of use thereof
WO2010075551A1 (en) * 2008-12-24 2010-07-01 Massachusetts Institute Of Technology Compositions of modulators of the wnt/beta-catenin pathway and benzamide and/or hydroxamic acid derivatives to treat bipolar disorder
WO2011019648A1 (en) * 2009-08-10 2011-02-17 Epitherix, Llc Indazoles as wnt/b-catenin signaling pathway inhibitors and therapeutic uses thereof
JP5763072B2 (ja) 2009-08-10 2015-08-12 サミュメッド リミテッド ライアビリティ カンパニー Wntシグナル経路のインダゾール阻害剤およびその治療的使用
EP2789615B1 (de) 2009-08-11 2017-05-03 Bristol-Myers Squibb Company Azaindazole als BTK-Kinasemodulatoren und Verwendung davon
RS56669B1 (sr) 2009-12-21 2018-03-30 Samumed Llc 1h-pirazolo[3,4-b]piridini i njihove terapeutske primene
MX354133B (es) 2010-08-18 2018-02-14 Samumed Llc Dicetonas e hidroxicetonas como activadores de la trayectoria de señalizacion de catenina.
ES2625534T3 (es) * 2011-04-25 2017-07-19 Usher Iii Initiative Pirazolopiridazinas y métodos para el tratamiento de enfermedades degenerativas de la retina y pérdida de la audición asociadas con el síndrome de Usher
WO2013010102A2 (en) 2011-07-14 2013-01-17 Latham Keith R Halogenated phenols for diagnostics, antioxidant protection and drug delivery
HUE041576T2 (hu) 2011-09-14 2019-05-28 Samumed Llc Indazol-3-karboxamid-származékok és alkalmazásuk Wnt/b-katenin szignalizáló útvonal inhibitorokként
US20150099645A1 (en) * 2012-03-14 2015-04-09 Stephen Marx Means and methods for diagnostics and therapeutics of diseases
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
NZ741907A (en) 2012-05-04 2020-02-28 Samumed Llc 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
ES2693166T3 (es) * 2012-10-25 2018-12-07 Usher Iii Initiative, Inc. Pirazolopiridina y métodos para tratar las enfermedades retinales degenerativas y la pérdida auditiva asociadas con el síndrome de Usher
US8765762B2 (en) 2012-10-25 2014-07-01 Usher III, Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degerative diseases and hearing loss associated with usher syndrome
US9227976B2 (en) 2012-10-25 2016-01-05 Usher Iii Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
CA2897400A1 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
EP3456325A3 (de) 2013-02-22 2019-05-22 Samumed, LLC Gamma-diketone als wnt/beta-catenin-signalisierungspfadaktivatoren
WO2015155738A2 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
SI3206686T1 (sl) 2014-08-20 2020-03-31 Samumed, Llc Gama-diketoni za zdravljenje in preprečevanje staranja kože in gub
WO2016040182A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040188A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10329309B2 (en) 2015-08-03 2019-06-25 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023984A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017023988A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023993A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024004A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017024025A1 (en) 2015-08-03 2017-02-09 Sunil Kumar Kc 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10226448B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
EP4541810A3 (de) * 2015-08-25 2026-03-18 Histide AG Verbindungen zur induktion von geweberegeneration und verwendungen davon
CN109311956A (zh) * 2015-08-25 2019-02-05 伊斯迪德股份公司 诱导组织形成的化合物及其应用
WO2017032857A2 (en) * 2015-08-25 2017-03-02 Histide Ag Compounds for inducing tissue formation and uses thereof
US10899757B2 (en) 2015-11-06 2021-01-26 Samumed, Llc 2-(1H-indazol-3-yl)-3H-imidazo[4,5-C]pyridines and their anti-inflammatory uses thereof
RS63813B1 (sr) 2016-06-01 2023-01-31 Biosplice Therapeutics Inc Postupak pripreme n-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida
RU2770613C2 (ru) 2016-10-21 2022-04-19 СЭМЬЮМЕД, ЭлЭлСи Способы применения индазол-3-карбоксамидов и их применение в качестве ингибиторов сигнального пути wnt/в-катенина
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
JP7352284B2 (ja) * 2017-05-15 2023-09-28 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン LSD-1インヒビターとしてのピロロ〔2,3-c〕ピリジン及び関連類似体
EP4178580B1 (de) 2020-07-09 2025-11-05 Usher III Initiative, Inc. Bf 844 zur verwendung bei der behandlung von krebs

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002024893A2 (en) * 2000-09-19 2002-03-28 Chiron Corporation CHARACTERIZATION OF THE GSK-3β PROTEIN AND METHODS OF USE THEREOF
WO2002050254A2 (en) * 2000-12-18 2002-06-27 Smithkline Beecham P.L.C. Crystal structure of glycogen synthase kinase 3 beta

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4009022A (en) 1975-10-30 1977-02-22 Rohm And Haas Company Selective antagonists for triazine herbicides
US4886646A (en) 1988-03-23 1989-12-12 The United States Of America As Represented By The Administrator Of The National Aeronautics And Space Administration Hanging drop crystal growth apparatus and method
US5096676A (en) 1989-01-27 1992-03-17 Mcpherson Alexander Crystal growing apparatus
US5130105A (en) * 1990-10-23 1992-07-14 The United States Of America As Represented By The Administrator Of The National Aeronautics And Space Administration Protein crystal growth tray assembly
US5200910A (en) 1991-01-30 1993-04-06 The Board Of Trustees Of The Leland Stanford University Method for modelling the electron density of a crystal
AU3320193A (en) 1991-07-22 1993-02-23 Regents Of The University Of California, The Methods of designing specific affectors using three-dimensional conformation of enzyme/affector complex
US5221410A (en) * 1991-10-09 1993-06-22 Schering Corporation Crystal forming device
US5353236A (en) * 1992-04-23 1994-10-04 The Board Of Trustees Of The Leland Stanford University High-resolution crystallographic modelling of a macromolecule
US5453937A (en) 1993-04-28 1995-09-26 Immunex Corporation Method and system for protein modeling
US5400741A (en) 1993-05-21 1995-03-28 Medical Foundation Of Buffalo, Inc. Device for growing crystals
EP1017823B1 (de) 1997-02-07 2004-07-14 Princeton University Veränderte proteinkinasen, die modifizierte nukleotidtriphosphat substrate verwenden können
GB9721437D0 (en) * 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
US6162613A (en) * 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
ATE274510T1 (de) 1998-06-19 2004-09-15 Chiron Corp Glycogen synthase kinase 3 inhibitoren
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
WO2000036096A1 (en) * 1998-12-16 2000-06-22 Vertex Pharmaceuticals Incorporated Crystallized p38 complexes
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
US7109199B2 (en) * 2000-09-22 2006-09-19 Smithkline Beecham Corporation Pyrazolopyridines and pyrazolopyridazines as antidiabetics
JP2005532265A (ja) * 2002-02-11 2005-10-27 カイロン コーポレイション ヒトgsk3を結晶化するための方法およびその新規な結晶構造
GB0206723D0 (en) * 2002-03-21 2002-05-01 Glaxo Group Ltd Novel compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002024893A2 (en) * 2000-09-19 2002-03-28 Chiron Corporation CHARACTERIZATION OF THE GSK-3β PROTEIN AND METHODS OF USE THEREOF
WO2002050254A2 (en) * 2000-12-18 2002-06-27 Smithkline Beecham P.L.C. Crystal structure of glycogen synthase kinase 3 beta

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
AOKI M ET AL: "EXPRESSION, PURIFICATION AND CRYSTALIZATION OF HUMAN TAU-PROTEIN KINASE I/GLYCOGEN SYNTHASE KINASE -3BETA", ACTA CRYSTALLOGRAPHICA SECTION D: BIOLOGICAL CRYSTALLOGRAPHY, MUNKSGAARD PUBLISHERS LTD. COPENHAGEN, DK, vol. 56, no. 11, November 2000 (2000-11-01), pages 1464 - 1465, XP001097943, ISSN: 0907-4449 *
DAJANI RANA ET AL: "Crystal structure of glycogen synthase kinase 3beta: Structural basis for phosphate-primed substrate specificity and autoinhibition", CELL, CELL PRESS, CAMBRIDGE, NA, US, vol. 105, no. 6, 15 June 2001 (2001-06-15), pages 721 - 732, XP002193600, ISSN: 0092-8674 *
TER HAAR E ET AL: "Structure of GSK3beta reveals a primed phosphorylation mechanism.", NATURE STRUCTURAL BIOLOGY. JUL 2001, vol. 8, no. 7, July 2001 (2001-07-01), pages 593 - 596, XP008042801, ISSN: 1072-8368 *

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AU2002259071A1 (en) 2002-11-11
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WO2002088078A2 (en) 2002-11-07
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EP1435957B1 (de) 2009-06-17
US7390808B2 (en) 2008-06-24
CA2444882A1 (en) 2002-11-07
US8318467B2 (en) 2012-11-27
US20030125332A1 (en) 2003-07-03
ATE433751T1 (de) 2009-07-15
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US7666647B2 (en) 2010-02-23
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